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奈非西坦药物的合成研究 被引量:2

Studies on Synthesis of Nefiracetam
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摘要 以碳酸钠为缚酸剂,摩尔比为1︰1的2,6-二甲基苯胺与氯乙酰氯反应合成了中间体2-氯-N-(2,6-二甲基苯基)乙酰胺;在强碱乙醇钠作用下,2-吡咯烷酮再与2-氯-N-(2,6-二甲基苯基)乙酰胺经亲核取代合成了目标化合物奈非西坦。探讨了影响中间体和奈非西坦产率的因素,在乙醇钠、2-氯-N-(2,6-二甲基苯基)乙酰胺和2-吡咯烷酮的摩尔比为2︰1︰2、反应时间为2 h的较佳工艺条件下,产品总收率达81%。 The 2-chloro-N-(2,6-dimethyl) phenyl acetamide was obtained from 2,6-dimethylaniline and chloroacetyl (molar ratio of 1 1) using sodium carbonate as antacid agent. Then sodium ethoxide was used as base, the nucleophilic substitution of 2-pyrrolidone with the intermediate provided nefiracetam. The influencing factors of the reaction yield were studied. The optimum reaction conditions were as follows: n(ethanol sodium) : n(2-chloro-N-(2,6-dimcthyl)phenyl acetamide) : n(2-pyrrolidonc) was 2 : 1 : 2 and reaction time was 2 h. The total yield of the product was 81%.
出处 《广东化工》 CAS 2007年第9期89-91,共3页 Guangdong Chemical Industry
基金 国家自然科学基金资助项目(No.20472080) 河南工业大学博士启动基金项目(No.150213)
关键词 奈非西坦 碳酸钠 2-氯.N-(2 6-二甲基苯基)乙酰胺 2-吡咯烷酮 乙醇钠 nefiracetam sodium carbonate 2-chloro-N-(2,6-dimethyl) phenyl acetamide 2-pyrrolidone sodium ethoxide
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